IP Library Granted Patent US 9,868,706
Granted Patent B2
US 9,868,706 · App. 15/406,476 · Granted Jan 16, 2018

Processes for the preparation of uracil derivatives

Inventors: Donald J. Gallagher (Hopkinton, MA); Laszlo R. Treiber (San Diego, CA); Robert Michael Hughes (San Diego, CA); Onorato Campopiano (Hayward, CA); Peng Wang (Carlsbad, CA); Yuxin Zhao (San Diego, CA); Shine K. Chou (Wildwood, MO); Michael Allen Ouellette (San Diego, CA); Donald Nicholas Hettinger (Broomfield, CO)
Assignee: Neurocrine Biosciences, Inc.
C07D239/54C07D239/553
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 9,868,706
App. No.
15/406,476
Granted
Jan 16, 2018
Kind
B2
Abstract

The present invention relates to processes and intermediates for preparing Gonadotropin-Releasing Hormone (GnRH) receptor antagonists of structure (VI); and stereoisomers and pharmaceutically acceptable salts thereof.

Claims (12)

1. A process for preparing a compound of structure:

wherein:

R 1a , R 1b and R 1c are the same or different and independently hydrogen, halogen, C 1-4 alkyl, hydroxy or alkoxy;

R 2a and R 2b are the same or different and independently hydrogen, halogen, trifluoromethyl, cyano or —SO 2 CH 3 ;

R 3 is hydrogen or methyl; and

comprising:

reacting a compound of structure (VII):

wherein R 2a , R 2b and R 3 are as defined above;

with a compound of structure (VIII):

wherein R is H or C 1-4 alkyl, R′ is H or C 1-4 alkyl or R and R′ taken together form C 1-6 alkanediyl; and

R 1a , R 1b , and R 1c are as defined above.

2. The process of claim 1 wherein R 1a is halogen, R 1b is methoxy and R 1c is H.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 6, 2019
From: GALLAGHER, DONALD J.; TREIBER, LASZLO R.; HUGHES, ROBERT MICHAEL; CAMPOPIANO, ONORATO; WANG, PENG; ZHAO, YUXIN; CHOU, HELEN; OUELLETTE, MICHAEL ALLEN; HETTINGER, DONALD NICHOLAS
To: NEUROCRINE BIOSCIENCES, INC.
Reel/Frame 048254/0383 →
Continuity (5)
Continuation 15174774 · Jun 6, 2016
Continuation 14309732 · Jun 19, 2014
Division 12741819
Provisional Application 60986227 · Nov 7, 2007
Related Publication 20170320836A1 · Nov 9, 2017